Work

Ocular delivery of repurposed everolimus against dry eye with a tear-triggered in situ hydrogel based on enhanced solubilization and retention

Year: 2026
Type: article
Abstract: ABSTRACT Dry eye represents an increasingly prominent public health burden in modern society. However, the limitations of currently available treatment options have necessitated the pursuit of new therapies. Here we report the repurposing of everolimus (Evero), an mTOR inhibitor with poor aqueous solubility, for dry eye management. Meanwhile, a tear-triggered in situ gelling system (EveroGel) based on the design principle of enhanced solubilization and retention was developed for topical administration of Evero. It was showed that the proposed formulation strategy can facilitate tissue permeation and decrease lacrimal clearance. Evero mitigated the severity of dry eye in a scopolamine-induced mouse model regarding corneal fluorescein, TUNEL, K10 immunofluorescent and conjunctival PAS staining. However, more favorable outcomes were obtained with EveroGel. All excipients present in EveroGel are FDA-approved. Hence, no toxic effects have been observed in the in vivo biocompatibility study. Our work demonstrates the therapeutic potential of rationally engineered ophthalmic formulations of Evero for treating dry eye.
Language: English
Open Access status: gold
Estimated APC paid: $3,400
Award: G771502911
OpenAlex ID: W7223696229
FWCI:
Cites: 76
Cited by:
Related to: 10